Assay Detail

CHEMBL4054685

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Binding

Displacement of [3H]-A-804598 from recombinant rat P2X7 expressed in human 1321N1 cells after 1 hr

ChEMBL ↗

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Target

P2X purinoceptor 7 (CHEMBL2496) ↗

Open DB target context

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P2X purinoceptor 7 (CHEMBL2496) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target P2X purinoceptor 7

CHEMBL2496

Anchored from Assay target.

Protein identity P2X purinoceptor 7

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Rattus norvegicus
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

P2X purinoceptor 7 (CHEMBL2496) ↗

Type	SINGLE PROTEIN
Organism	Rattus norvegicus

Publication

4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate.

Letavic MA, Savall BM, Allison BD, Aluisio L, Andres JI, De Angelis M, Ao H, Beauchamp DA, Bonaventure P, Bryant S, Carruthers NI, Ceusters M, Coe KJ, Dvorak CA, Fraser IC, Gelin CF, Koudriakova T, Liang J, Lord B, Lovenberg TW, Otieno MA, Schoetens F, Swanson DM, Wang Q, Wickenden AD, Bhattacharya A.
J Med Chem (2017) 60 : 4559 -4572
PubMed 28493698 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	1	8.30	8.30

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4079239	JNJ-54175446	2.0	1	8.30

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4079239	JNJ-54175446	Ki	=	5.012	nM	8.30